IS2980B - Methods for Preparation of 4 - [[4 - [[4- (2-cyanoethyl) -2,6-dimethylphenyl] amino] -2-pyrimidinyl] amino] benzonitrile - Google Patents
Methods for Preparation of 4 - [[4 - [[4- (2-cyanoethyl) -2,6-dimethylphenyl] amino] -2-pyrimidinyl] amino] benzonitrileInfo
- Publication number
- IS2980B IS2980B IS7621A IS7621A IS2980B IS 2980 B IS2980 B IS 2980B IS 7621 A IS7621 A IS 7621A IS 7621 A IS7621 A IS 7621A IS 2980 B IS2980 B IS 2980B
- Authority
- IS
- Iceland
- Prior art keywords
- amino
- cyanoethyl
- benzonitrile
- dimethylphenyl
- pyrimidinyl
- Prior art date
Links
- FXOGXMVMRGLWIG-UHFFFAOYSA-N 4-[[4-[4-(2-cyanoethyl)-2,6-dimethylanilino]pyrimidin-2-yl]amino]benzonitrile Chemical compound CC1=CC(CCC#N)=CC(C)=C1NC1=CC=NC(NC=2C=CC(=CC=2)C#N)=N1 FXOGXMVMRGLWIG-UHFFFAOYSA-N 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C253/00—Preparation of carboxylic acid nitriles
- C07C253/20—Preparation of carboxylic acid nitriles by dehydration of carboxylic acid amides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C253/00—Preparation of carboxylic acid nitriles
- C07C253/30—Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pharmacology & Pharmacy (AREA)
- Oncology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP02078306 | 2002-08-09 | ||
PCT/EP2003/050366 WO2004016581A1 (en) | 2002-08-09 | 2003-08-07 | Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile |
Publications (2)
Publication Number | Publication Date |
---|---|
IS7621A IS7621A (en) | 2004-12-29 |
IS2980B true IS2980B (en) | 2017-09-15 |
Family
ID=31725448
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
IS7621A IS2980B (en) | 2002-08-09 | 2004-12-29 | Methods for Preparation of 4 - [[4 - [[4- (2-cyanoethyl) -2,6-dimethylphenyl] amino] -2-pyrimidinyl] amino] benzonitrile |
Country Status (26)
Country | Link |
---|---|
US (3) | US7399856B2 (en) |
EP (1) | EP1529032B1 (en) |
JP (1) | JP4822707B2 (en) |
KR (2) | KR101140785B1 (en) |
CN (4) | CN100554245C (en) |
AR (1) | AR040964A1 (en) |
AU (1) | AU2003266413B2 (en) |
CA (2) | CA2493794C (en) |
CL (1) | CL2010000284A1 (en) |
CY (1) | CY1114428T1 (en) |
DK (1) | DK1529032T3 (en) |
EA (1) | EA007953B1 (en) |
ES (1) | ES2422196T3 (en) |
HK (4) | HK1081527A1 (en) |
HR (1) | HRP20050104B1 (en) |
IL (1) | IL166710A (en) |
IS (1) | IS2980B (en) |
MX (1) | MXPA05001541A (en) |
MY (1) | MY144894A (en) |
NO (1) | NO330013B1 (en) |
NZ (1) | NZ538611A (en) |
PL (1) | PL208533B1 (en) |
PT (1) | PT1529032E (en) |
SI (1) | SI1529032T1 (en) |
TW (1) | TWI314146B (en) |
WO (1) | WO2004016581A1 (en) |
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
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US7638522B2 (en) * | 2001-08-13 | 2009-12-29 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino] benzonitrile |
MY169670A (en) | 2003-09-03 | 2019-05-08 | Tibotec Pharm Ltd | Combinations of a pyrimidine containing nnrti with rt inhibitors |
JO3429B1 (en) | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | Hiv inhibiting pyrimidines derivatives |
US8101629B2 (en) * | 2001-08-13 | 2012-01-24 | Janssen Pharmaceutica N.V. | Salt of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile |
EP1529032B1 (en) * | 2002-08-09 | 2013-04-24 | Janssen Pharmaceutica NV | Processes for the preparation of 4- 4- 4-(2 -cyanoethenyl)-2,6-dimethylphenyl )amino) -2-pyrimidinyl)amino benzonitrile |
US7504410B2 (en) * | 2002-11-28 | 2009-03-17 | Schering Aktiengesellschaft | Chk-, Pdk- and Akt-inhibitory pyrimidines, their production and use as pharmaceutical agents |
WO2005123662A1 (en) * | 2004-06-18 | 2005-12-29 | Janssen Pharmaceutica N.V. | Modified heck reaction |
JP4922937B2 (en) * | 2004-09-02 | 2012-04-25 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 4-((4-((4- (2-cyanoethenyl) -2,6-dimethylphenyl) amino) -2-pyrimidinyl) amino) benzonitrile fumarate |
AU2005279157B2 (en) * | 2004-09-02 | 2011-07-14 | Janssen Pharmaceutica N.V. | Fumarate of 4-[[4-[[4- (2-cyanoethenyl) -2,6-dimethylphenyl]amino)-2-pyrimidinyl)amino]benzonitrile |
RS51923B2 (en) * | 2004-09-02 | 2022-05-31 | Janssen Pharmaceutica Nv | Salt of [[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyi]amino]-2-, pyrimidinyl]amino]benzonitrile |
CA2577288C (en) * | 2004-09-02 | 2010-11-30 | Janssen Pharmaceutica N.V. | Hydrochloride of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile |
AP2296A (en) * | 2004-09-02 | 2011-10-31 | Janssen Pharmaceutica Nv | Hydrochloride of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile. |
US7314962B2 (en) * | 2005-04-15 | 2008-01-01 | E. I. Du Pont De Nemours & Co. | Alkylation of aromatic compounds |
EP1888537B1 (en) * | 2005-05-26 | 2013-09-11 | Janssen R&D Ireland | Process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)amino benzonitrile |
CL2008000746A1 (en) | 2007-03-14 | 2008-09-22 | Tibotec Pharm Ltd | PHARMACEUTICAL COMPOSITION IN SOLUTION INCLUDING TMC278 AND A WATER SOLUBLE POLYMER; PREPARATION PROCESS OF SUCH COMPOSITION; AND USE OF A POWDER UNDERSTANDING TMC278 TO TREAT AIDS. |
AU2008274185B2 (en) * | 2007-07-12 | 2014-07-03 | Janssen Sciences Ireland Uc | Crystalline form of (E) 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2 pyrimidinyl]amino]benzonitrile |
WO2012125993A1 (en) | 2011-03-17 | 2012-09-20 | Teva Pharmaceutical Industries Ltd. | Solid state forms of rilpivirine base, and rilipivirine salts |
AP2013006779A0 (en) * | 2011-04-15 | 2013-03-31 | Emcure Pharmaceuticals Ltd | An improved rilpivirine process |
EP2702044B1 (en) | 2011-04-25 | 2017-03-22 | Hetero Research Foundation | Process for rilpivirine |
CA2848631C (en) | 2011-09-16 | 2019-10-01 | Hetero Research Foundation | Rilpivirine hydrochloride |
WO2013170421A1 (en) * | 2012-05-14 | 2013-11-21 | 上海迪赛诺药业有限公司 | Rilpivirine hydrochloride alcoholate polymorph and preparation method thereof |
WO2013179105A1 (en) * | 2012-06-01 | 2013-12-05 | Laurus Labs Private Limited | Improved process for preparation of rilpivirine and pharmaceutically acceptable salts thereof |
WO2014009968A2 (en) * | 2012-07-12 | 2014-01-16 | Hetero Research Foundation | Process for rilpivirine using novel intermediate |
CZ201532A3 (en) | 2015-01-21 | 2015-02-25 | Zentiva, K.S. | Process for preparing extremely pure rilpivirine and salt thereof |
CN106008366A (en) * | 2016-05-25 | 2016-10-12 | 山东大学 | Preparation method of rilpivirine |
BR112019007564A2 (en) | 2016-10-24 | 2019-07-02 | Janssen Sciences Ireland Unlimited Company | dispersible compositions |
EP3870568B1 (en) | 2018-10-25 | 2023-06-28 | Minakem | Process for the preparation of rilpivirine |
CN110526873B (en) * | 2019-08-15 | 2022-09-16 | 复旦大学 | Cyanovinyl substituted benzodiarylpyrimidine compound and preparation method and application thereof |
US11166952B2 (en) | 2019-11-29 | 2021-11-09 | Aptorum Therapeutics Limited | Composition including rilpivirine and method for treating tumors or cancer |
CN112010810B (en) * | 2020-09-09 | 2024-01-30 | 瑞阳制药股份有限公司 | Method for preparing high-purity rilpivirine intermediate by one-pot method |
CN112778214A (en) * | 2021-01-13 | 2021-05-11 | 安徽贝克联合制药有限公司 | Intermediate for synthesizing rilpivirine, synthesis method thereof and rilpivirine synthesis method |
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MY169670A (en) | 2003-09-03 | 2019-05-08 | Tibotec Pharm Ltd | Combinations of a pyrimidine containing nnrti with rt inhibitors |
JO3429B1 (en) * | 2001-08-13 | 2019-10-20 | Janssen Pharmaceutica Nv | Hiv inhibiting pyrimidines derivatives |
TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
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EP1529032B1 (en) | 2002-08-09 | 2013-04-24 | Janssen Pharmaceutica NV | Processes for the preparation of 4- 4- 4-(2 -cyanoethenyl)-2,6-dimethylphenyl )amino) -2-pyrimidinyl)amino benzonitrile |
WO2004050068A1 (en) | 2002-11-29 | 2004-06-17 | Janssen Pharmaceutica N.V. | Pharmaceutical compositions comprising a basic respectively acidic drug compound, a surfactant and a physiologically tolerable water-soluble acid respectively base |
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2003
- 2003-08-07 EP EP03787813.9A patent/EP1529032B1/en not_active Expired - Lifetime
- 2003-08-07 CN CNB038192764A patent/CN100554245C/en not_active Expired - Lifetime
- 2003-08-07 CN CN2011101114129A patent/CN102225902B/en not_active Expired - Lifetime
- 2003-08-07 CN CN201210159781.XA patent/CN102702111B/en not_active Expired - Lifetime
- 2003-08-07 NZ NZ538611A patent/NZ538611A/en not_active IP Right Cessation
- 2003-08-07 CA CA2493794A patent/CA2493794C/en not_active Expired - Lifetime
- 2003-08-07 DK DK03787813.9T patent/DK1529032T3/en active
- 2003-08-07 KR KR1020057000881A patent/KR101140785B1/en active IP Right Grant
- 2003-08-07 MX MXPA05001541A patent/MXPA05001541A/en active IP Right Grant
- 2003-08-07 PT PT37878139T patent/PT1529032E/en unknown
- 2003-08-07 EA EA200500325A patent/EA007953B1/en unknown
- 2003-08-07 PL PL373679A patent/PL208533B1/en unknown
- 2003-08-07 MY MYPI20032999A patent/MY144894A/en unknown
- 2003-08-07 CA CA2686429A patent/CA2686429C/en not_active Expired - Lifetime
- 2003-08-07 CN CN200910001327XA patent/CN101481356B/en not_active Expired - Lifetime
- 2003-08-07 US US10/523,753 patent/US7399856B2/en not_active Expired - Lifetime
- 2003-08-07 AU AU2003266413A patent/AU2003266413B2/en not_active Expired
- 2003-08-07 JP JP2004528518A patent/JP4822707B2/en not_active Expired - Lifetime
- 2003-08-07 KR KR1020107026275A patent/KR101086678B1/en active IP Right Grant
- 2003-08-07 ES ES03787813T patent/ES2422196T3/en not_active Expired - Lifetime
- 2003-08-07 WO PCT/EP2003/050366 patent/WO2004016581A1/en active Application Filing
- 2003-08-07 SI SI200332275T patent/SI1529032T1/en unknown
- 2003-08-08 AR ARP030102882A patent/AR040964A1/en active IP Right Grant
- 2003-08-08 TW TW092121743A patent/TWI314146B/en not_active IP Right Cessation
-
2004
- 2004-12-29 IS IS7621A patent/IS2980B/en unknown
-
2005
- 2005-02-01 HR HRP20050104AA patent/HRP20050104B1/en not_active IP Right Cessation
- 2005-02-01 NO NO20050524A patent/NO330013B1/en not_active IP Right Cessation
- 2005-02-07 IL IL166710A patent/IL166710A/en active Protection Beyond IP Right Term
-
2006
- 2006-02-09 HK HK06101734.3A patent/HK1081527A1/en not_active IP Right Cessation
- 2006-02-09 HK HK09108307.2A patent/HK1129671A1/en not_active IP Right Cessation
-
2007
- 2007-04-23 US US11/738,688 patent/US7563922B2/en active Active
-
2008
- 2008-02-14 US US12/031,011 patent/US7705148B2/en active Active
-
2010
- 2010-03-29 CL CL2010000284A patent/CL2010000284A1/en unknown
-
2012
- 2012-02-23 HK HK12101815.7A patent/HK1161869A1/en not_active IP Right Cessation
-
2013
- 2013-02-25 HK HK13102335.5A patent/HK1174922A1/en not_active IP Right Cessation
- 2013-07-24 CY CY20131100631T patent/CY1114428T1/en unknown
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